I-CBP112，≥98% (HPLC)

I-CBP112 has been used in cell culture and sample preparation,[1] to verify the acetylation of VPS34 (vacuolar protein sorting 34), by p300 at K29, K771 and K781[2] and to diminish synergistic gene expression.[3]

 

I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC₅₀ = 0.142 and 0.625 μM, respectively). I-CBP112 has little activity against other bromodomains at concentrations up to 1 mM. For full characterization details, please see I-CBP112 on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

I-CBP112 is also known as (1-[7-(3,4-dimethoxyphenyl)-9-{[(3S)-1-methylpiperidin-3-yl]-methoxy}-2,3,4,5-tetrahydro-1,4-benzoxazepin-4-yl]propan-1-one). It has the ability to induce full-length p300/CBP nucleosome acetylation.[4] It is a competitive inhibitor of acetyl-lysine. I-CBP112 regulates transcription of key inflammatory genes.[5]

 

I-CBP112 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

 

I-CBP112 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the I-CBP112 probe summary on the Chemical Probes Portal website.